GDC-0326

GDC-0326 is an inhibitor of phosphatidylinositol 3-kinase alpha (PI3Kalpha, Ki = 0.2 nM) that is 133-, 20-, and 51-fold selective for PI3Kalpha over PI3Kbeta, PI3Kdelta, and PI3Kgamma, respectively. It inhibits proliferation of MCF7-neo/HER2 and PC3 cells (EC50s = 0.1 and 2.2 µM, respectively). In vivo, GDC-0326 (6.25 mg/kg) induces tumor regression in a KPL-4 mouse xenograft model. It also reduces tumor growth, tumor vasculature, and the number of liver and lymph node metastases in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors.Formal Name: (2S)-2-[[5,6-dihydro-2-[1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9-yl]oxy]-propanamide. CAS Number: 1282514-88-8. Molecular Formula: C19H22N6O3. Formula Weight: 382.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: Slightly soluble. lambdamax: 276, 306 nm. SMILES: O=C(N)[C@H](C)OC1=CC=C(C2=NC(C3=NC=NN3C(C)C)=CN2CCO4)C4=C1. InChi Code: InChI=1S/C19H22N6O3/c1-11(2)25-19(21-10-22-25)15-9-24-6-7-27-16-8-13(28-12(3)17(20)26)4-5-14(16)18(24)23-15/h4-5,8-12H,6-7H2,1-3H3,(H2,20,26)/t12-/m0/s1. InChi Key: SIKYDKLGPWRPMZ-LBPRGKRZSA-N.